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BX430 is a selective noncompetitive allosteric antagonist of human P2X4 receptor channels. P2X4 receptors are highly expressed in the CNS, and have been studied as a therapeutic target for neuropathic pain and inflammation, and treatment of traumatic brain injury, cerebral ischemia, and spinal cord injury. BX430 is highly selective for human P2X4, with minimal activity towards other P2X subtypes, including P2X1–P2X3, P2X5, and P2X7. BX430 is also an antagonist of zebrafish P2X4 but has no effect on rat and mouse P2X4 receptors. BX430 has an IC50 value of 540 nM.

Biperiden hydrochloride is antiparkinsonian; non-selective muscarinic receptor antagonist. It is used for the adjunctive treatment of all forms of Parkinson′s Disease (postencephalitic, idiopathic, and arteriosclerotic); also commonly used to improve parkinsonian signs and symptoms related to antipsychotic drug therapy. LD50 in rats 750 mg/kg; in dogs 340 mg/kg.

JNJ-47965567 is a potent P2X7 antagonist with high affinity for the rat receptor (pKi = 8.7). It is centrally available after systemic injection with a superior brain:plasma distribution compared to other available P2X7 antagonists. JNJ-47965567 was shown to suppress epileptic seizures in a mouse model of epilepsy. It appears to have a disease modifying effect since spontaneous seizure rates did not increase once treatment with JNJ-477965567 was stopped.

MRS 1191 is putative A3 adenosine receptor antagonist, highly selective for human A3 receptor vs human A1 receptor. MRS 1067, MRS 1191 and MRS 1220 were found to be competitive in saturation binding studies using the agonist radioligand [125I]AB-MECA at cloned human brain A3 receptors expressed in HEK-293 cells. Antagonism was demonstrated in functional assays consisting of agonist-induced inhibition of adenylate cyclase and the stimulation of binding of [35S]guanosine 5′-O-(3-thiotriphosphate) ([35S]GTP-gamma-S) to the associated G-proteins. Activation of the human A3 receptor in A3R-CHO results in markedly impaired cell cycle progression, suggesting an important role for this adenosine receptor subtype in cell cycle regulation and cell growth. Activation of adenosine A3 receptors by Cl-IBMECA (100 nM) increased the magnitude of theta-burst induced LTP (from 1.2+/-0.6% in the control solution to 25.5+/-0.8% in the presence of Cl-IBMECA) and attenuated LTD (from 30.0+/-5.5% decrease in the control solution to 13.6+/-6.6% decrease in the presence of Cl-IBMECA). The selective adenosine A3 receptor antagonist, MRS 1191 (5-10 μM), prevented the effects of Cl-IBMECA. These findings indicate a functional role for adenosine A3 receptors in the modulation of synaptic plasticity.

Prasugrel is a platelet inhibitor that reduces the aggregation of platelets by irreversible binding to P2Y12 receptors. Prasugrel interacts in an irreversible manner with the residues Cys97 and Cys175 of the human P2Y12-receptor.

Reversine was first described as a synthetic substituted purine with activity as a dedifferentiation agent; it was shown to induces differentiated lineage-committed cells to become multipotent mesenchymal stem cells (MSCs). Reversine has also been show to have activity as a potent, selective human A3 adenosine receptor antagonist (Ki value of 0.66 μM), as an ATP-competitive Aurora kinase inhibitor, and as a Mps1 kinase inhibitor. Additionally, studies have shown reversine to be an anti-cancer agent, inhibiting growth and inducing cell death in various cancer cell types.

A2A adenosine receptor antagonist.SCH 58261 reduces the levels of TNF-α, Fas-L, Bax expression and activation of JNK-MAPK pathway. It has neuroprotective effects as it reduces demyelination of the neurons. SCH 58261 increases the concentration of secretion of dopamine and elicits locomotor sensitization, an attractive option in the possible treatment of Parkinson′s disease.

ZM 241385 is a potent selective adenosine A2A antagonist. The A2A receptor plays a role in regulating myocardial oxygen consumption and coronary blood flow and is highly expressed in the brain, where it has important roles in the regulation of glutamate and dopamine release. ZM 241385 has neuroprotective effects and is being investigated for use in Parkinson′s and other neurodegenerative disorders.